Biological Activity
Inhibitor of p38 MAP kinase (IC50 = 0.1 - 1 μM). Potently inhibits LPS-induced IL-1 and TNF-α production in human monocytes (IC50 = 1 μM). Also inhibits 5-lipoxygenase- and cyclooxygenase-mediated arachidonic acid metabolism in RBL-1 cells (IC50 values are 10 and 100 μM respectively). Anti-inflammatory following oral administration in vivo.
Technical Data
| M. Wt | 370.27 |
| Formula | C16H12FN3S.2HCl |
| Storage | Desiccate at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 116339-68-5 |
| PubChem ID | 10339107 |
| InChI Key | GQQCNUNCYVXBTF-UHFFFAOYSA-N |
| Smiles | Cl.Cl.FC1=CC=C(C=C1)C1=C(N2CCSC2=N1)C1=CC=NC=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 18.51 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 370.27. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.7 mL | 13.5 mL | 27.01 mL |
| 5 mM | 0.54 mL | 2.7 mL | 5.4 mL |
| 10 mM | 0.27 mL | 1.35 mL | 2.7 mL |
| 50 mM | 0.05 mL | 0.27 mL | 0.54 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Griswold et al (1987) SK&F 86002: a structurally novel anti-inflammatory agent that inhibits lipoxygenase- and cyclooxygenase-mediated metabolism of arachidonic acid. Biochem.Pharmacol. 36 3463 PMID: 2823821
Lee et al (1994) A protein kinase involved in the regulaton of inflammatory cytokine biosynthesis. Nature 372 739 PMID: 7997261
Nick et al (1997) Common and distinct intracellular signaling pathways in human neutrophils utilized by platelet activating factor and FMLP. J.Clin.Invest. 99 975 PMID: 9062356
Keywords: SKF 86002 dihydrochloride, supplier, p38, MAP, kinases, inhibitors, inhibits, anti-inflammatory, agent, human, monocyte, IL-1, TNF-α, TNF-alpha, production, Mitogen-Activated, Protein, Kinase, MAPK, Signaling, Signalling, Interleukins, Tumor, Necrosis, Factor-α, Factor-alpha, Cytokines, SKF86002, dihydrochl, p38, Cytokines, p38, Tocris Bioscience
